EP0846721A1 - Utilisation de mélatonine dans une composition pour stabiliser les polyméres gélifiants hydrophiles - Google Patents
Utilisation de mélatonine dans une composition pour stabiliser les polyméres gélifiants hydrophiles Download PDFInfo
- Publication number
- EP0846721A1 EP0846721A1 EP97402686A EP97402686A EP0846721A1 EP 0846721 A1 EP0846721 A1 EP 0846721A1 EP 97402686 A EP97402686 A EP 97402686A EP 97402686 A EP97402686 A EP 97402686A EP 0846721 A1 EP0846721 A1 EP 0846721A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- melatonin
- polymer
- composition
- hydrophilic
- hydrophilic gelling
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/04—Dispersions; Emulsions
- A61K8/042—Gels
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
- A61K8/4913—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid
- A61K8/492—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid having condensed rings, e.g. indol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q5/00—Preparations for care of the hair
- A61Q5/06—Preparations for styling the hair, e.g. by temporary shaping or colouring
- A61Q5/065—Preparations for temporary colouring the hair, e.g. direct dyes
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08K—Use of inorganic or non-macromolecular organic substances as compounding ingredients
- C08K5/00—Use of organic ingredients
- C08K5/16—Nitrogen-containing compounds
- C08K5/34—Heterocyclic compounds having nitrogen in the ring
- C08K5/3412—Heterocyclic compounds having nitrogen in the ring having one nitrogen atom in the ring
- C08K5/3415—Five-membered rings
- C08K5/3417—Five-membered rings condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/52—Stabilizers
Definitions
- the present invention relates to the use of melatonin or its analogs for stabilizing compositions comprising gelling polymers hydrophilic, in particular in cosmetic compositions or topical pharmaceuticals.
- Hydrophilic gelling agents are widely used in topical cosmetic or pharmaceutical compositions. These include gelling agents such as polymers of natural and / or synthetic origin, among which mention may be made of carboxyvinyl polymers (carbomers), acrylic copolymers such as acrylate / alkyl acrylate copolymers, polyacrylamides or optionally modified polysaccharides such as hydroxypropylcellulose.
- carboxyvinyl polymers carboxyvinyl polymers
- acrylic copolymers such as acrylate / alkyl acrylate copolymers
- polyacrylamides such as hydroxypropylcellulose.
- melatonin or its analogues made it possible to stabilize the hydrophilic gelling polymers, in preventing their loss of viscosity under the action of light.
- Melatonin or N-acetyl-5-methoxytriptamine, secreted by the pineal gland, is best known for its circadian activity regulating production hormones, especially for its influence on sleep patterns.
- compositions comprising melatonin for use therapeutic or cosmetic have been described, such as toilet lotions, toilet creams or milks (JP-A-61-221104).
- the article by Bangha & al. concerning the effectiveness of melatonin in suppressing erythema induced by U.V.B also describes the use of melatonin in a gel of nanocolloids. Melatonin is still used as an active agent, no document not describing or suggesting its influence on the stability of polymers hydrophilic gelling agents. It is also notable that melatonin is used in these compositions essentially for its antioxidant properties, in particular for the capture of free radicals, when it is not a molecule filtering in the solar spectrum, between 280 and 800 nm.
- the present invention therefore relates to the use of melatonin or of at least one of its analogs for stabilizing the compositions comprising at least one hydrophilic gelling polymer.
- stabilize we essentially mean prevent their loss of viscosity under the action of light.
- analogues of melatonin there may be mentioned in particular its derivatives, such as 5-methoxytryptamine, 5-methoxytryptophan, 5-methoxytryptophol, 5-methoxyindole-3-acetic acid and 6-hydroxymelatonin.
- melatoninergic agonists such as those described in patent applications WO-A-95/17405, EP-A-0447285, EP-A-0527687, EP-A-0530087 and EP-A-0591057. These compounds can be of natural or synthetic origin.
- melatonin will be used.
- hydrophilic gelling polymers the following are advantageously understood: polymers of natural and / or synthetic origin, among which mention may be made of carboxyvinyl polymers (carbomer), acrylic copolymers such as copolymers of acrylates / alkylacrylates, polyacrylamides or polysaccharides, such as guar gum, xanthan gum or celluloses, possibly modified like hydroxypropylcellulose. It can also be a mixture of these polymers.
- carboxyvinyl polymers carboxyvinyl polymers (carbomer)
- acrylic copolymers such as copolymers of acrylates / alkylacrylates
- polyacrylamides or polysaccharides such as guar gum, xanthan gum or celluloses, possibly modified like hydroxypropylcellulose. It can also be a mixture of these polymers.
- the hydrophilic gelling polymer is a polymer carboxyvinyl, for example marketed under the brand name Carbopol® by the GOODRICH company.
- Topical compositions must contain a medium topically acceptable, i.e. compatible with the skin, mucous membranes, nails, scalp and hair.
- the present invention also relates to a method for stabilizing a composition
- a composition comprising at least one hydrophilic gelling polymer, consisting of add an appropriate amount of melatonin or at least one of its analogs to prevent loss of viscosity of said polymer under the action of light.
- the weight ratio of melatonin or its analogs the hydrophilic gelling polymer is between 1/2000 and 20/1, preferably between 1/500 and 1/2.
- the present invention finally relates to cosmetic compositions or pharmaceutical, in particular topical, comprising at least one polymer hydrophilic gelling agent and as stabilizing agent for said gelling polymer hydrophilic, melatonin or at least one of its analogs.
- compositions comprise between 0.001% and 0.2% by weight of melatonin or its analogs and between 0.01% and 3% by weight of hydrophilic gelling polymer. The percentage by weight is expressed relative to the total weight of the composition.
- compositions containing melatonin or its analogues can be presented in all dosage forms for topical use normally used comprising at least one hydrophilic gelling agent, under the form in particular of aqueous solution, emulsions of liquid or semi-liquid consistency of the milk type, or of suspensions or emulsions of soft consistency of the type aqueous cream or gel.
- hydrophilic gelling agent under the form in particular of aqueous solution, emulsions of liquid or semi-liquid consistency of the milk type, or of suspensions or emulsions of soft consistency of the type aqueous cream or gel.
- compositions constitute in particular cleaning, protection creams, of treatment or care for the face, for the hands, for the feet, for the large anatomical or body folds (e.g. day creams, night, make-up removing creams, foundation creams, sun creams), fluid complexions, cleansing milks, body protection or care milks, sun milks, lotions, gels or foams for skin care, such as cleaning lotions, sun lotions, artificial tanning lotions, bath compositions, deodorant compositions comprising an agent bactericide, aftershave gels or lotions, depilatory creams, insect bite compositions, pain relieving compositions, compositions for treating certain skin diseases such as eczema, rosacea, psoriasis, lichens, severe pruritus.
- skin care e.g. day creams, night, make-up removing creams, foundation creams, sun creams
- fluid complexions e.g. day creams, night, make-up removing creams, foundation creams, sun cream
- the cosmetic or dermatological composition may contain also usual adjuvants in the cosmetic or dermatological field, such as preservatives, antioxidants, solvents, fragrances, fillers, filters, odor absorbers and coloring matter.
- adjuvants such as preservatives, antioxidants, solvents, fragrances, fillers, filters, odor absorbers and coloring matter.
- the quantities of these various adjuvants are those conventionally used in these fields, and by example from 0.01% to 10% of the total weight of the composition.
- the composition may contain hydrophilic active agents such as proteins or protein hydrolysates, amino acids, polyols, urea, allantoin, sugars and sugar derivatives, water-soluble vitamins, plant extracts and hydroxy acids, or active ingredients intended in particular for prevention and / or treatment skin conditions such as agents that modulate differentiation and / or proliferation and / or skin pigmentation, antibacterials, antiparasitics, antifungals, steroidal or non-steroidal anti-inflammatory agents, antipruritic agents, anti-free radical agents, antiseborrheics such as progesterone, CGRP antagonists or substance P antagonists or again the bradykinin antagonists, and the dandruff agents.
- hydrophilic active agents such as proteins or protein hydrolysates, amino acids, polyols, urea, allantoin, sugars and sugar derivatives, water-soluble vitamins, plant extracts and hydroxy acids, or active ingredients intended in particular for prevention and / or treatment skin conditions such as agents that modulate differentiation and /
- Example 1 comprising a hydrophilic gelling polymer and melatonin has been subjected to UV exposure (including wavelengths between 300 and 830 nm) in a closed SUNTEST CPS-HERAEUS enclosure, the samples being packaged in bare glass vials.
- composition 1 The viscosity of composition 1 was measured before exposure, after 4 hours exposure and after 19 hours of exposure and compared to that of the same composition not comprising melatonin (Control). The measurements were performed at RHEOMAT 108 E / R at constant temperature (25 ° C) and the reading was done after 10 minutes of shearing on mobile 3 and mobile 2.
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Birds (AREA)
- Dispersion Chemistry (AREA)
- Dermatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Polymers & Plastics (AREA)
- Organic Chemistry (AREA)
- Cosmetics (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Carbomer commercialisé sous la dénomination Carbopol 940 par la société GOODRICH | 0,50 % |
Triéthanolamine | 0,50 % |
Mélatonine | 0,18 % |
Conservateurs | qs |
Colorants | qs |
Eau | qsp 100 % |
Stéarate de glycérol | 0,50 % |
PEG 100 stéarate | 2,00 % |
Alcool cétylique | 0,40 % |
Cyclométhicone | 3,00 % |
Huile de soja | 3,00 % |
Acrylates/C10-C30 alkyl acrylate crosspolymère (CTFA) commercialisé sous la dénomination Carbopol 1382 par la société GOODRICH | 0,30 % |
Mélatonine | 0,05 % |
Conservateurs | qs |
Eau | qsp 100 % |
Sodium laureth sulfate | 2,00 % |
Glycérine | 3,00 % |
Carbomer commercialisé sous la dénomination Carbopol 940 par la société GOODRICH | 0,20 % |
Carraghenane | 0,30 % |
Hydroxyde de sodium | 0,10 % |
Mélatonine | 0,03 % |
Conservateurs | qs |
Eau | qsp 100 % |
Viscosité | Témoin | Composition de l'exemple 1 |
Avant exposition U.V. | 37,5 Poises (M3) | 40 Poises (M3) |
Après 4 heures d'exposition | 14 Poises (M3) (Diminution de viscosité 62 %) | 28 Poises (M3) (Diminution de viscosité 30 %) |
Après 19 heures d'exposition | 2,5 Poises (M2) (Diminution de viscosité 93 %) | 16 Poises (M3) (Diminution de viscosité 60 %) |
Claims (10)
- Utilisation de la mélatonine ou d'au moins un de ses analogues pour stabiliser une composition comprenant au moins un polymère gélifiant hydrophile, pour prévenir la perte de viscosité dudit polymère sous l'action de la lumière.
- Utilisation selon la revendication 1, caractérisée en ce que l'analogue de la mélatonine est choisi parmi la 5-méthoxytryptamine, 5-méthoxytryptophane, 5-méthoxytryptophol, l'acide 5-méthoxyindole-3-acétique, la 6-hydroxymélatonine et leurs mélanges.
- Utilisation selon la revendication 1, caractérisée en ce que l'on utilise la mélatonine.
- Utilisation selon l'une des revendications 1 à 3, caractérisée en ce que le polymère gélifiant hydrophile est choisi parmi les polymères carboxyvinyliques (carbomer), les copolymères acryliques, les polyacrylamides, les polysaccharides éventuellement modifiés et leurs mélanges.
- Utilisation selon la revendication 5, caractérisée en ce que le polymère gélifiant hydrophile est un polymère carboxyvinylique.
- Utilisation selon l'une des revendications 1 à 5, caractérisée en ce que le rapport pondéral de la mélatonine ou de son analogue au polymère gélifiant hydrophile est compris entre 1/2000 et 20/1, de préférence compris entre 1/500 et 1/2.
- Utilisation selon l'une des revendications 1 à 6, caractérisée en ce que la composition est une composition cosmétique ou pharmaceutique.
- Procédé de stabilisation d'une composition comprenant au moins un polymère gélifiant hydrophile, consistant à ajouter une quantité approprié de mélatonine ou d'au moins un de ses analogues pour prévenir la perte de viscosité dudit polymère sous l'action de la lumière.
- Composition cosmétique ou pharmaceutique comprenant au moins un polymère gélifiant hydrophile, caractérisée en ce qu'elle comprend, à titre d'agent de stabilisation dudit polymère gélifiant hydrophile, de la mélatonine ou au moins un de ses analogues.
- Composition selon la revendication 9, caractérisée en ce qu'elle comprend entre 0,001% et 0,2% en poids de mélatonine ou ses analogues et entre 0,01% et 3% en poids de polymère gélifiant hydrophile, par rapport au poids total de la composition.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9615045 | 1996-12-06 | ||
FR9615045A FR2756832B1 (fr) | 1996-12-06 | 1996-12-06 | Utilisation de melatonine dans une composition pour stabiliser les polymeres gelifiants hydrophiles |
Publications (2)
Publication Number | Publication Date |
---|---|
EP0846721A1 true EP0846721A1 (fr) | 1998-06-10 |
EP0846721B1 EP0846721B1 (fr) | 2002-06-05 |
Family
ID=9498437
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP97402686A Expired - Lifetime EP0846721B1 (fr) | 1996-12-06 | 1997-11-10 | Utilisation de mélatonine dans une composition pour stabiliser les polyméres gélifiants hydrophiles |
Country Status (5)
Country | Link |
---|---|
US (1) | US5891903A (fr) |
EP (1) | EP0846721B1 (fr) |
DE (1) | DE69713035T2 (fr) |
ES (1) | ES2177915T3 (fr) |
FR (1) | FR2756832B1 (fr) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE19957710A1 (de) * | 1999-11-30 | 2001-05-31 | Asat Ag Applied Science & Tech | Verwendung von Melatonin zur Behandlung der androgenetischen Alopezie |
EP2179739A1 (fr) * | 2008-10-23 | 2010-04-28 | Matteo Tutino | Compositions comportant des vitamines |
CN111053735A (zh) * | 2020-02-25 | 2020-04-24 | 上海阶平医院管理有限公司 | 一种治疗失眠的冷敷凝胶 |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CH470385A (de) * | 1963-06-06 | 1969-03-31 | Merck & Co Inc | Verfahren zur Herstellung von Indolylsäuren |
EP0438856A2 (fr) * | 1989-10-31 | 1991-07-31 | Shiseido Company Limited | Utilisation de la mélatonine pour protéger la peau contre les effets des rayons U-V |
EP0714968A2 (fr) * | 1994-12-02 | 1996-06-05 | Ucc Ueshima Coffee Co., Ltd. | Antioxydant naturel et procédé pour sa préparation |
WO1997006779A1 (fr) * | 1995-08-11 | 1997-02-27 | Kistler Gonzague S | Protection contre les dommages cutanes induits par rayonnements ultraviolets (uv) a l'aide d'un traitement topique faisant appel a de la melatonine (n-acetyl-5-methoxytryptamine) |
FR2741799A1 (fr) * | 1995-12-04 | 1997-06-06 | Oreal | Utilisation de melatonine dans une composition pour traiter les signes cutanes des etats de fatigue |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5688520A (en) * | 1995-03-29 | 1997-11-18 | Minnesota Mining And Manufacturing Company | Transmucosal delivery of melatonin for prevention of migraine |
-
1996
- 1996-12-06 FR FR9615045A patent/FR2756832B1/fr not_active Expired - Fee Related
-
1997
- 1997-11-10 DE DE69713035T patent/DE69713035T2/de not_active Expired - Fee Related
- 1997-11-10 EP EP97402686A patent/EP0846721B1/fr not_active Expired - Lifetime
- 1997-11-10 ES ES97402686T patent/ES2177915T3/es not_active Expired - Lifetime
- 1997-12-08 US US08/986,516 patent/US5891903A/en not_active Expired - Fee Related
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CH470385A (de) * | 1963-06-06 | 1969-03-31 | Merck & Co Inc | Verfahren zur Herstellung von Indolylsäuren |
EP0438856A2 (fr) * | 1989-10-31 | 1991-07-31 | Shiseido Company Limited | Utilisation de la mélatonine pour protéger la peau contre les effets des rayons U-V |
EP0714968A2 (fr) * | 1994-12-02 | 1996-06-05 | Ucc Ueshima Coffee Co., Ltd. | Antioxydant naturel et procédé pour sa préparation |
WO1997006779A1 (fr) * | 1995-08-11 | 1997-02-27 | Kistler Gonzague S | Protection contre les dommages cutanes induits par rayonnements ultraviolets (uv) a l'aide d'un traitement topique faisant appel a de la melatonine (n-acetyl-5-methoxytryptamine) |
FR2741799A1 (fr) * | 1995-12-04 | 1997-06-06 | Oreal | Utilisation de melatonine dans une composition pour traiter les signes cutanes des etats de fatigue |
Also Published As
Publication number | Publication date |
---|---|
ES2177915T3 (es) | 2002-12-16 |
EP0846721B1 (fr) | 2002-06-05 |
FR2756832B1 (fr) | 1999-01-08 |
DE69713035D1 (de) | 2002-07-11 |
FR2756832A1 (fr) | 1998-06-12 |
US5891903A (en) | 1999-04-06 |
DE69713035T2 (de) | 2002-09-19 |
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